GSK931145

GSK931145 is a **selective inhibitor** of the glycine transporter type 1 (GlyT1) developed by GSK. It has primarily been used as a radiolabeled ligand ([11C]GSK931145, [3H]GSK931145) for positron emission tomography (PET) studies to image GlyT1 distribution and occupancy in the brain. GlyT1 is a transporter involved in glycine reuptake in the central nervous system, relevant to glutamatergic neurotransmission. Inhibition of GlyT1 is of therapeutic interest as a potential treatment for schizophrenia. GSK931145 itself has shown good brain penetration and high specific binding in preclinical and early clinical imaging studies, but was primarily evaluated as a PET probe rather than as a therapeutic agent. It is a small molecule chemical drug and also classified as a diagnostic radiopharmaceutical when labeled with radioisotopes such as carbon-11 ([11C]) or tritium ([3H]) for imaging purposes[1][2][3][4][5][7][9].

Other names

[3H]GSK931145[11C]GSK931145